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Ashok Kumar - One of the best experts on this subject based on the ideXlab platform.
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synthesis of some newer derivatives of substituted quinazolinonyl 2 oxo thiobarbituric acid as potent anticonvulsant agents
Bioorganic & Medicinal Chemistry, 2004Co-Authors: V K Srivastava, Ashok KumarAbstract:Abstract 5-{1′-[3″-Aminoacetyl-2″-methyl-6″,8″-dihalosubstitutedquinazolin-4″(3″H)-onyl]-thiosemicarbazido}-2-oxo/thiobarbituric acids 3a – 3h and 5-{2′-amino-5′-[3″-aminomethylene-2″-methyl-6″,8″-dihalosubstitutedquinazolin-4″(3″H)-onyl]-1′,3′,4′-thiadiazol-2′-yl}-2-oxo/thiobarbituric acid 5a – 5h were prepared by incorporating 1-[3′-aminoacetyl-2′-methyl-6″,8″-dihalosubstituted-quinazolin-4′(3′H)-onyl]-Thiosemicarbazides 2a – 2d and 2-amino-5-[3′-aminomethylene-2′-methyl-6′,8′-dihalosubstituted-quinazolin-4′(3′H)-onyl]-1,3,4-thiadiazoles 4a-4 h respectively at 5 th position of 2-oxo/thiobarbituric acids (via Mannich reaction). All the newly synthesized compounds were screened for their anti-convulsant activity in MES and PTZ models and were compared with standard drugs phenytoin sodium and sodium valproate. Interestingly, these compounds were found to be devoid of sedative and hypnotic activities when tested. Out of the compounds studied, the most active compound 5h , that is 5-{2′-amino-5′-[3″-aminomethylene-2″-methyl-6″,8″-dibromoquinazolin-4″(3″H)-onyl]-1′,3′,4′-thiadiazol-2′-yl}-2-thiobarbituric acid showed activity (90%) more potent than the standard drug.
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Synthesis of some newer derivatives of substituted quinazolinonyl-2-oxo/thiobarbituric acid as potent anticonvulsant agents.
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Archana, Vishnu Srivastava, Ashok KumarAbstract:Abstract 5-{1′-[3″-Aminoacetyl-2″-methyl-6″,8″-dihalosubstitutedquinazolin-4″(3″H)-onyl]-thiosemicarbazido}-2-oxo/thiobarbituric acids 3a – 3h and 5-{2′-amino-5′-[3″-aminomethylene-2″-methyl-6″,8″-dihalosubstitutedquinazolin-4″(3″H)-onyl]-1′,3′,4′-thiadiazol-2′-yl}-2-oxo/thiobarbituric acid 5a – 5h were prepared by incorporating 1-[3′-aminoacetyl-2′-methyl-6″,8″-dihalosubstituted-quinazolin-4′(3′H)-onyl]-Thiosemicarbazides 2a – 2d and 2-amino-5-[3′-aminomethylene-2′-methyl-6′,8′-dihalosubstituted-quinazolin-4′(3′H)-onyl]-1,3,4-thiadiazoles 4a-4 h respectively at 5 th position of 2-oxo/thiobarbituric acids (via Mannich reaction). All the newly synthesized compounds were screened for their anti-convulsant activity in MES and PTZ models and were compared with standard drugs phenytoin sodium and sodium valproate. Interestingly, these compounds were found to be devoid of sedative and hypnotic activities when tested. Out of the compounds studied, the most active compound 5h , that is 5-{2′-amino-5′-[3″-aminomethylene-2″-methyl-6″,8″-dibromoquinazolin-4″(3″H)-onyl]-1′,3′,4′-thiadiazol-2′-yl}-2-thiobarbituric acid showed activity (90%) more potent than the standard drug.
V K Srivastava - One of the best experts on this subject based on the ideXlab platform.
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synthesis of some newer derivatives of substituted quinazolinonyl 2 oxo thiobarbituric acid as potent anticonvulsant agents
Bioorganic & Medicinal Chemistry, 2004Co-Authors: V K Srivastava, Ashok KumarAbstract:Abstract 5-{1′-[3″-Aminoacetyl-2″-methyl-6″,8″-dihalosubstitutedquinazolin-4″(3″H)-onyl]-thiosemicarbazido}-2-oxo/thiobarbituric acids 3a – 3h and 5-{2′-amino-5′-[3″-aminomethylene-2″-methyl-6″,8″-dihalosubstitutedquinazolin-4″(3″H)-onyl]-1′,3′,4′-thiadiazol-2′-yl}-2-oxo/thiobarbituric acid 5a – 5h were prepared by incorporating 1-[3′-aminoacetyl-2′-methyl-6″,8″-dihalosubstituted-quinazolin-4′(3′H)-onyl]-Thiosemicarbazides 2a – 2d and 2-amino-5-[3′-aminomethylene-2′-methyl-6′,8′-dihalosubstituted-quinazolin-4′(3′H)-onyl]-1,3,4-thiadiazoles 4a-4 h respectively at 5 th position of 2-oxo/thiobarbituric acids (via Mannich reaction). All the newly synthesized compounds were screened for their anti-convulsant activity in MES and PTZ models and were compared with standard drugs phenytoin sodium and sodium valproate. Interestingly, these compounds were found to be devoid of sedative and hypnotic activities when tested. Out of the compounds studied, the most active compound 5h , that is 5-{2′-amino-5′-[3″-aminomethylene-2″-methyl-6″,8″-dibromoquinazolin-4″(3″H)-onyl]-1′,3′,4′-thiadiazol-2′-yl}-2-thiobarbituric acid showed activity (90%) more potent than the standard drug.
Archana - One of the best experts on this subject based on the ideXlab platform.
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Synthesis of some newer derivatives of substituted quinazolinonyl-2-oxo/thiobarbituric acid as potent anticonvulsant agents.
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Archana, Vishnu Srivastava, Ashok KumarAbstract:Abstract 5-{1′-[3″-Aminoacetyl-2″-methyl-6″,8″-dihalosubstitutedquinazolin-4″(3″H)-onyl]-thiosemicarbazido}-2-oxo/thiobarbituric acids 3a – 3h and 5-{2′-amino-5′-[3″-aminomethylene-2″-methyl-6″,8″-dihalosubstitutedquinazolin-4″(3″H)-onyl]-1′,3′,4′-thiadiazol-2′-yl}-2-oxo/thiobarbituric acid 5a – 5h were prepared by incorporating 1-[3′-aminoacetyl-2′-methyl-6″,8″-dihalosubstituted-quinazolin-4′(3′H)-onyl]-Thiosemicarbazides 2a – 2d and 2-amino-5-[3′-aminomethylene-2′-methyl-6′,8′-dihalosubstituted-quinazolin-4′(3′H)-onyl]-1,3,4-thiadiazoles 4a-4 h respectively at 5 th position of 2-oxo/thiobarbituric acids (via Mannich reaction). All the newly synthesized compounds were screened for their anti-convulsant activity in MES and PTZ models and were compared with standard drugs phenytoin sodium and sodium valproate. Interestingly, these compounds were found to be devoid of sedative and hypnotic activities when tested. Out of the compounds studied, the most active compound 5h , that is 5-{2′-amino-5′-[3″-aminomethylene-2″-methyl-6″,8″-dibromoquinazolin-4″(3″H)-onyl]-1′,3′,4′-thiadiazol-2′-yl}-2-thiobarbituric acid showed activity (90%) more potent than the standard drug.
Vishnu Srivastava - One of the best experts on this subject based on the ideXlab platform.
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Synthesis of some newer derivatives of substituted quinazolinonyl-2-oxo/thiobarbituric acid as potent anticonvulsant agents.
Bioorganic & Medicinal Chemistry, 2004Co-Authors: Archana, Vishnu Srivastava, Ashok KumarAbstract:Abstract 5-{1′-[3″-Aminoacetyl-2″-methyl-6″,8″-dihalosubstitutedquinazolin-4″(3″H)-onyl]-thiosemicarbazido}-2-oxo/thiobarbituric acids 3a – 3h and 5-{2′-amino-5′-[3″-aminomethylene-2″-methyl-6″,8″-dihalosubstitutedquinazolin-4″(3″H)-onyl]-1′,3′,4′-thiadiazol-2′-yl}-2-oxo/thiobarbituric acid 5a – 5h were prepared by incorporating 1-[3′-aminoacetyl-2′-methyl-6″,8″-dihalosubstituted-quinazolin-4′(3′H)-onyl]-Thiosemicarbazides 2a – 2d and 2-amino-5-[3′-aminomethylene-2′-methyl-6′,8′-dihalosubstituted-quinazolin-4′(3′H)-onyl]-1,3,4-thiadiazoles 4a-4 h respectively at 5 th position of 2-oxo/thiobarbituric acids (via Mannich reaction). All the newly synthesized compounds were screened for their anti-convulsant activity in MES and PTZ models and were compared with standard drugs phenytoin sodium and sodium valproate. Interestingly, these compounds were found to be devoid of sedative and hypnotic activities when tested. Out of the compounds studied, the most active compound 5h , that is 5-{2′-amino-5′-[3″-aminomethylene-2″-methyl-6″,8″-dibromoquinazolin-4″(3″H)-onyl]-1′,3′,4′-thiadiazol-2′-yl}-2-thiobarbituric acid showed activity (90%) more potent than the standard drug.
Ulrich Abram - One of the best experts on this subject based on the ideXlab platform.
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neutral gold complexes with tridentate sns Thiosemicarbazide ligands
Inorganic Chemistry, 2012Co-Authors: Pedro I. S. Maia, Hung Huy Nguyen, Victor M. Deflon, Daniela Ponader, Adelheid Hagenbach, Silke Bergemann, Ronald Gust, Ulrich AbramAbstract:Na[AuCl4]·2H2O reacts with tridentate Thiosemicarbazide ligands, H2L1, derived from N-[N′,N′-dialkylamino(thiocarbonyl)]benzimidoyl chloride and Thiosemicarbazides under formation of air-stable, green [AuCl(L1)] complexes. The organic ligands coordinate in a planar SNS coordination mode. Small amounts of gold(I) complexes of the composition [AuCl(L3)] are formed as side-products, where L3 is an S-bonded 5-diethylamino-3-phenyl-1-thiocarbamoyl-1,2,4-triazole. The formation of the triazole L3 can be explained by the oxidation of H2L1 to an intermediate thiatriazine L2 by Au3+, followed by a desulfurization reaction with ring contraction. The chloro ligands in the [AuCl(L1)] complexes can readily be replaced by other monoanionic ligands such as SCN– or CN– giving [Au(SCN)(L1)] or [Au(CN)(L1)] complexes. The complexes described in this paper represent the first examples of fully characterized neutral Gold(III) thiosemicarbazone complexes. All the [AuCl(L1)] compounds present a remarkable cell growth inhibitio...
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Oxotechnetium(V) complexes with a novel class of tridentate Thiosemicarbazide ligands.
Inorganic chemistry, 2009Co-Authors: Hung Huy Nguyen, Pedro I. S. Maia, Victor M. Deflon, Ulrich AbramAbstract:A novel tridentate Thiosemicarbazide-type ligand class with an SNS donor set, H2L1, was prepared by reactions of N-[N′,N′-dialkylamino(thiocarbonyl)]benzimidoyl chlorides with Thiosemicarbazides. H2L1 ligands readily react with (NBu4)[TcOCl4] in MeOH under the formation of red oxotechnetium(V) complexes of composition [TcOCl(L1)]. The monomeric, five-coordinate compounds are air-stable and bind (L1)2− tridentate in the equatorial coordination sphere. The compounds represent the first examples of oxotechnetium(V) complexes with NS chelate-bonded thiosemicarbazones.
